Topical ophthalmic peptide formulation

Abstract

A topical ophthalmic formulation of peptides and their use for the treatment and/or local prevention of ocular diseases, preferably posterior segment eye diseases.

The invention claimed is: 
     
       1. A method of treatment of a posterior segment of eye disease selected from the group consisting of nonproliferative diabetic retinopathy, proliferative diabetic retinopathy, retinal neurodegeneration, retinal neovascularization, ischemia-induced retinopathy, retinopathy of prematurity, sickle-cell retinopathy, retinal vein occlusion, retinitis pigmentosa and combinations thereof, comprising:
 administering topically a therapeutically effective amount of somatostatin or a somatostatin analogue selected from the group consisting of somatostatin-28, somatostatin-14, somatostatin-13, prosomatostatin, octreotide, lanreotide, vapreotide, pasireotide, seglitide, cortistatin, and pharmaceutically acceptable salts thereof, by a topical ophthalmic composition selected from the group consisting of eye drops, ointments and unguents, wherein the concentration of the somatostatin or somatostatin analogue ranges between 1 μg/mL and 40 mg/mL, and wherein the composition is an isotonic aqueous solution, a poly(vinyl alcohol) aqueous solution, or mixtures thereof of pH between 3 and 8. 
 
     
     
       2. The method according to  claim 1 , wherein the somatostatin or somatostatin analogue is substituted with an acyl group or a polyethylene glycol moiety. 
     
     
       3. The method according to  claim 1 , wherein the concentration ranges between 1 μg/mL and 10 mg/mL. 
     
     
       4. The method according to  claim 1 , wherein the ophthalmic composition further comprises a preservative. 
     
     
       5. The method according to  claim 4 , wherein the preservative is selected from the group consisting of benzalkonium chloride, benzoic acid, alkyl parabens, alkyl benzoates, chlorobutanol, chlorocresol, cetyl alcohols, fatty alcohols, hexadecyl alcohol, organometallic compounds of mercury, mercury acetate, phenylmercury nitrate or borate, diazolidinyl urea, diisopropyl adipate, dimethyl polysiloxane, salts of EDTA, vitamin E and mixtures thereof. 
     
     
       6. The method according to  claim 1 , wherein the ophthalmic composition further comprises an agent that increases permeability of the somatostatin or somatostatin analogue. 
     
     
       7. The method according to  claim 6 , wherein the agent that increases permeability is selected from the group consisting of benzalkonium chloride, saponins, fatty acids, polyoxyethylene fatty ethers, alkyl esters of fatty acids, pyrrolidones, polyvinylpyrrolidone, pyruvic acids, pyroglutamic acids, and mixtures thereof. 
     
     
       8. The method according to  claim 1 , wherein the somatostatin or somatostatin analogue is incorporated in liposomes, mixed liposomes, niosomes, ethosomes, nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, micelles, mixed micelles of surfactants, surfactant-phospholipid mixed micelles, nanospheres, lipospheres and/or nanocapsules. 
     
     
       9. The method according to  claim 1 , wherein the treatment of posterior segment of eye diseases benefits from binding of somatostatin or somatostatin analogue to somatostatin receptors.